Allosteric modulation of class A GPCRs: targets, agents, and emerging concepts

EA Wold, J Chen, KA Cunningham… - Journal of medicinal …, 2018 - ACS Publications
G-protein-coupled receptors (GPCRs) have been tractable drug targets for decades with
over one-third of currently marketed drugs targeting GPCRs. Of these, the class A GPCR …

[HTML][HTML] Research progress of indole-fused derivatives as allosteric modulators: opportunities for drug development

ML Luo, Q Zhao, XH He, X Xie, HP Zhu, FM You… - Biomedicine & …, 2023 - Elsevier
Allosteric modulation is a direct and effective method for regulating the function of biological
macromolecules, which play vital roles in various cellular activities. Unlike orthosteric …

Widespread receptor-driven modulation in peripheral olfactory coding

L Xu, W Li, V Voleti, DJ Zou, EMC Hillman, S Firestein - Science, 2020 - science.org
INTRODUCTION The mammalian nose is arguably the best chemical sensor on the planet,
able to detect and discriminate among a large and diverse repertoire of mostly small …

Discovery of Novel Oleamide Analogues as Brain-Penetrant Positive Allosteric Serotonin 5-HT2C Receptor and Dual 5-HT2C/5-HT2A Receptor Modulators

J Chen, EJ Garcia, CR Merritt, JC Zamora… - Journal of medicinal …, 2023 - ACS Publications
The serotonin 5-HT2A receptor (5-HT2AR) and 5-HT2CR localize to the brain and share
overlapping signal transduction facets that contribute to their roles in cognition, mood …

Allosteric modulation of a human odorant receptor

C Trimmer, R Arroyave, C Vuilleumier, L Wu, A Dumer… - Current Biology, 2023 - cell.com
Odor perception is first determined by how the myriad of environmental volatiles are
detected at the periphery of the olfactory system. The combinatorial activation of dedicated …

Targeting the 5-HT2C receptor in biological context and the current state of 5-HT2C receptor ligand development

EA Wold, CT Wild, KA Cunningham… - Current topics in …, 2019 - ingentaconnect.com
Serotonin (5-HT) 5-HT2C receptor (5-HT2CR) is recognized as a critical mediator of
diseaserelated pathways and behaviors based upon actions in the central nervous system …

Molecular and structural insights into the 5‐HT2C receptor as a therapeutic target for substance use disorders

M Ubhayarathna, CJ Langmead… - British Journal of …, 2024 - Wiley Online Library
Substance use disorder (SUD) is a chronic condition, with maintained abuse of a substance
leading to physiological and psychological alterations and often changes in cognitive and …

Allosteric modulators of G protein-coupled dopamine and serotonin receptors: a new class of atypical antipsychotics

I Fasciani, F Petragnano, G Aloisi, F Marampon… - Pharmaceuticals, 2020 - mdpi.com
Schizophrenia was first described by Emil Krapelin in the 19th century as one of the major
mental illnesses causing disability worldwide. Since the introduction of chlorpromazine in …

Odor mixtures: A chord with silent notes

L Xu, DJ Zou, S Firestein - Frontiers in Ecology and Evolution, 2023 - frontiersin.org
The olfactory world is one of complex mixtures and blends containing up to hundreds of
molecules. Many of those molecules can act as agonists, antagonists or enhancers at …

Therapeutic potential of allosteric modulators for the treatment of gastrointestinal motility disorders

A Saito, S Alvi, C Valant… - British Journal of …, 2024 - Wiley Online Library
Gastrointestinal motility is tightly regulated by the enteric nervous system (ENS). Disruption
of coordinated enteric nervous system activity can result in dysmotility. Pharmacological …